Title: Synthesis and in vitro enzymatic and antiviral evaluation of phosphoramidate d4T derivatives as chain terminators
Authors: Yang, Shiqiong
Pannecouque, Christophe
Lescrinier, Eveline
Giraut, Anne
Herdewijn, Piet # ×
Issue Date: Jan-2012
Publisher: Royal Society of Chemistry
Series Title: Organic & Biomolecular Chemistry vol:10 issue:1 pages:146-153
Abstract: The anti-HIV activity of nucleoside analogues is highly related to their substrate specificity for cellular and viral kinase and, as triphosphate, for HIV-RT. A series of phosphoramidate d4T derivatives have been synthesized and evaluated as substrates for HIV-1 RT, and also tested for their in vitro anti-HIV activity. Compounds 2 and 4 are able to inhibit HIV-1 replication to the same extent as d4T and d4TMP in MT-4 cells as well as in CEM/0 cells and CEM/TK(-) cells. The data suggests that these phosphoramidates are hydrolysed to d4T before exerting their antiviral activity.
ISSN: 1477-0520
Publication status: published
KU Leuven publication type: IT
Appears in Collections:Medicinal Chemistry (Rega Institute)
× corresponding author
# (joint) last author

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